Date published: 2025-10-19

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Astemizole (CAS 68844-77-9)

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Alternate Names:
Hismanal;1-[(4-Fluorophenyl)methyl]-N-[1-[2-(4-methoxyphenyl)ethyl]-4-piperidinyl]-1H-benzimidazol-2-amine
Application:
Astemizole is a potent and selective H1-receptor antagonist that displays antihistamine and antimalarial activity
CAS Number:
68844-77-9
Purity:
≥97%
Molecular Weight:
458.58
Molecular Formula:
C28H31FN4O
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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Astemizole is a compound that has been the subject of various research studies due to its interaction with histamine receptors and other biological targets. In scientific investigations, it is often used as a tool to probe the function of the histamine H1 receptor, helping to elucidate the complex signaling pathways associated with histamine response. Moreover, Astemizole is known for its ability to inhibit certain potassium channels, which has made it valuable in cardiac electrophysiology studies, where researchers aim to understand the ionic currents contributing to the cardiac action potential. Outside of its known histamine receptor affinity, Astemizole has also been utilized in studies exploring its potential impact on other cellular processes, including its off-target effects.


Astemizole (CAS 68844-77-9) References

  1. Reversal of acquired resistance to doxorubicin in K562 human leukemia cells by astemizole.  |  Ishikawa, M., et al. 2000. Biol Pharm Bull. 23: 112-5. PMID: 10706423
  2. The binding site for channel blockers that rescue misprocessed human long QT syndrome type 2 ether-a-gogo-related gene (HERG) mutations.  |  Ficker, E., et al. 2002. J Biol Chem. 277: 4989-98. PMID: 11741928
  3. A clinical drug library screen identifies astemizole as an antimalarial agent.  |  Chong, CR., et al. 2006. Nat Chem Biol. 2: 415-6. PMID: 16816845
  4. Pharmacological separation of hEAG and hERG K+ channel function in the human mammary carcinoma cell line MCF-7.  |  Roy, J., et al. 2008. Oncol Rep. 19: 1511-6. PMID: 18497958
  5. Intracellular potassium stabilizes human ether-à-go-go-related gene channels for export from endoplasmic reticulum.  |  Wang, L., et al. 2009. Mol Pharmacol. 75: 927-37. PMID: 19139152
  6. Astemizole analogues with reduced hERG inhibition as potent antimalarial compounds.  |  Tian, J., et al. 2017. Bioorg Med Chem. 25: 6332-6344. PMID: 29042223
  7. Astemizole Inhibits mTOR Signaling and Angiogenesis by Blocking Cholesterol Trafficking.  |  Lyu, J., et al. 2018. Int J Biol Sci. 14: 1175-1185. PMID: 30123067
  8. Astemizole-based turn-on fluorescent probes for imaging hERG potassium channel.  |  Zhang, X., et al. 2019. Medchemcomm. 10: 513-516. PMID: 31057730
  9. Astemizole Sensitizes Adrenocortical Carcinoma Cells to Doxorubicin by Inhibiting Patched Drug Efflux Activity.  |  Hasanovic, A., et al. 2020. Biomedicines. 8: PMID: 32751066
  10. Cryo-EM Structure of K+-Bound hERG Channel Complexed with the Blocker Astemizole.  |  Asai, T., et al. 2021. Structure. 29: 203-212.e4. PMID: 33450182
  11. Astemizole as a drug to inhibit the effect of SARS-COV-2 in vitro.  |  Wang, X., et al. 2021. Microb Pathog. 156: 104929. PMID: 33932547
  12. In vitro and in vivo binding characteristics of a new long-acting histamine H1 antagonist, astemizole.  |  Laduron, PM., et al. 1982. Mol Pharmacol. 21: 294-300. PMID: 6124876
  13. Astemizole. A review of its pharmacodynamic properties and therapeutic efficacy.  |  Richards, DM., et al. 1984. Drugs. 28: 38-61. PMID: 6204835

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

Astemizole, 10 mg

sc-201088
10 mg
$113.00

Astemizole, 50 mg

sc-201088A
50 mg
$404.00